The present invention relates to 1,2,4-triazole heterocyclic carbon compounds, their preparation, metabolic transformations and use. More particularly, the invention relates to keto and triazoldione analogs of the antidepressant agent nefazodone.
Nefazodone is a member of a series of compounds having structure (1) as disclosed by Temple, Jr., et al. in U.S. Pat. No. 4,338,317. ##STR1## Nefazodone (R is meta-chloro) has been extensively studied clinically as an antidepressant agent.
A major metabolic pathway for nefazodone and related analogs involves .alpha.-carbon hydroxylation of the ethyl group attached to the 5-position of the triazolone ring. These antidepressant compounds as well as certain ether and ester derivatives were disclosed and claimed in U.S. Pat. No. 4,613,600 as structure (2). In these compounds, Z is ##STR2## hydrogen or phenoxy and R.sup.1 is, inter alia, an alkyl or acyl moiety.